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Submit ReviewSunitinib malate is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor (Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively). Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models.
Sold for research purposes under agreement from Pfizer Inc.
Sunitinib malate is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 532.56 |
公式 | C22H27FN4O2.C4H6O5 |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 341031-54-7 |
PubChem ID | 6456015 |
InChI Key | LBWFXVZLPYTWQI-IPOVEDGCSA-N |
Smiles | O=C(NCCN(CC)CC)C1=C(C)NC(/C=C2\C(NC3=C2C=C(F)C=C3)=O)=C1C.OC(C[C@H](O)C(O)=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 13.31 | 25 |
以下数据基于产品分子量 532.56。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.25 mM | 7.51 mL | 37.55 mL | 75.11 mL |
1.25 mM | 1.5 mL | 7.51 mL | 15.02 mL |
2.5 mM | 0.75 mL | 3.76 mL | 7.51 mL |
12.5 mM | 0.15 mL | 0.75 mL | 1.5 mL |
参考文献是支持产品生物活性的出版物。
Mendel et al (2003) In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin.Cancer Res. 9 327 PMID: 12538485
O'Farrell et al (2003) SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood 101 3597 PMID: 12531805
Faivre et al (2007) Molecular basis for suni. efficacy and future clinical development Nat.Rev.Drug Discov. 6 734 PMID: 17690708
Roskoski (2007) Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor. Biochem.Biophys.Res.Comm. 356 323 PMID: 17367763
If you know of a relevant reference for Sunitinib malate, please let us know.
关键词: Sunitinib malate, Sunitinib malate supplier, Potent, VEGFR, PDGRb, PDGFRbeta, PDGFRβ, FGFR, inhibitors, inhibits, Vascular, Endothelial, Growth, Factor, Receptors, KDR, Flt, Flk, Kit, Receptor, Tyrosine, Kinases, RTKs, Fibroblast, platelet, derived, CD117, SU11248, Pfizer, SU, 11248, PDGFR, Other, 3768, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Sunitinib malate 的部分引用包括:
Procaccia et al (2014) Gleevec/imatinib, an ABL2 kinase inhibitor, protects tumor and endothelial cells from semaphorin-induced cytoskeleton collapse and loss of cell motility. Biochem Biophys Res Commun 448 134 PMID: 24759231
Goel et al (2014) VEGF???-conjugated mesoporous silica nanoparticle: a tumor targeted drug delivery system. ACS Appl Mater Interfaces 6 21677 PMID: 25353068
Gaji et al (2014) Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother 58 2598 PMID: 24550330
Mathew et al (2015) Feedback circuitry between miR-218 repression and RTK activation in glioblastoma. Cell Death Differ 8 ra42 PMID: 25943352
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